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  • Title: Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.
    Author: Salvati ME, Balog A, Shan W, Rampulla R, Giese S, Mitt T, Furch JA, Vite GD, Attar RM, Jure-Kunkel M, Geng J, Rizzo CA, Gottardis MM, Krystek SR, Gougoutas J, Galella MA, Obermeier M, Fura A, Chandrasena G.
    Journal: Bioorg Med Chem Lett; 2008 Mar 15; 18(6):1910-5. PubMed ID: 18291644.
    Abstract:
    A novel series of [2.2.1]-oxabicyclo imide-based compounds were identified as potent antagonists of the androgen receptor. Molecular modeling and iterative drug design were applied to optimize this series. The lead compound [3aS-(3aalpha,4beta,5beta,7beta,7aalpha)]-4-(octahydro-5-hydroxy-4,7-dimethyl-1,3-dioxo-4,7-epoxy-2H-isoindol-2-yl)-2-iodobenzonitrile was shown to have potent in vivo efficacy after oral dosing in the CWR22 human prostate tumor xenograph model.
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